Nurr1 agonist 29

Chemical Structure : Nurr1 agonist 29

加入收藏

货号: PC-20768Not For Human Use, Lab Use Only.

Nurr1 agonist 29 is a potent, selective nuclear receptor related 1 (Nurr1, NR4A2) agonist with EC50 of 0.11 uM.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote
1 g		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

Nurr1 agonist 29 is a potent, selective nuclear receptor related 1 (Nurr1, NR4A2) agonist with EC50 of 0.11 uM.
Nurr1 agonist 29 displays selectivity over DHODH as well as the Nurr1 related receptors Nur77 and NOR1.
Nurr1 agonist 29 exhibits high-affinity binding to the Nurr1 LBD in ITC (Kd = 0.3 μM) and activates full-length human Nurr1 on the monomer (NBRE, EC50=0.22 μM) and the RXR-heterodimer (DR5, EC50=0.36 μM) response elements.
Nurr1 agonist 29 induces mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) in Nurr1-expressing human astrocytes (T98G), demonstrating cellular target engagement.
Nurr1 agonist 29 shows no cytotoxic effects in a multiplex toxicity assay in COS-7 cells.
Nurr1 agonist 29 (5 mg/kg) produced a very favorable pharmacokinetic profile in rats with a 4.4 h half-life, 56 μM peak plasma concentration, and 89% bioavailability.

物理化学性质&存储条件

分子量	379.39
分子式	C22H18FNO4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	O=C(C1=C(C(NC2=CC=C(C3=CC=CC(OCC#C)=C3)C=C2F)=O)CCC1)O

参考文献

1. Jan Vietor, et al. Journal of Medicinal Chemistry, April 26, 2023

Nurr1 agonist 29

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Nurr1 agonist 29

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.